Erythromycin A, used for the treatment of gram positive infections in man, has a relatively short serum half-life of from 2 to 3 hours. This half-life makes multiple doses necessary during each treatment day to maintain a bacterial inhibitory serum concentration. To provide greater patient convenience and to facilitate patient compliance with a prescribed course of antibiotic therapy, it would be desirable to have an erythromycin form which can be effectively administered on a once- or twice-a-day schedule.
Erythromycin, like most antibiotics, has a limited antimicrobial spectrum. In addition, bacteria spontaneously acquire resistance to antibiotics through repeated exposure to nonlethal concentrations of the drug. Such resistant strains eventually predominate, particularly in hospital populations, rendering the antibiotics ineffective. It would be desirable to have an erythromycin-based antibiotic which has a broader antimicrobial spectrum than erythromycin. It would also be desirable for such a drug to be effective against erythromycin-resistant bacteria.
The present invention relates to a compound (and derivatives thereof) having improved antibacterial activity and prolonged serum half-life. The result is an antibiotic composition which can be administered once or twice each day in the treatment or prevention of a broad range of bacterial infections.
U.S. Pat. No. 3,417,077, issued in 1968 to H. W. Murphy et al. discloses erythromycin A 11,12-carbonate.
Japanese Patent Publication No. 58-49,396 (Toyo Jozo Company Ltd., 1983) discloses 4"-deoxyerythromycin A.